Lithium derivative medicament

ABSTRACT

LITHIUM PARACHLOROPHENOXYACETATE IS A NOVEL MEDICAMENT ACTIVE IN THE TREATMENT OF MENTAL DISEASES. IT IS PREPARED BY REACTING PARACHLOROPHENOXYACETIC ACID WITH LITHIUM CARBONATE.

United States Patent 3,803,322 LITHIUM DERIVATIVE MEDICAMENT Jean-ClaudeDenis and Jerome Rambaud, Paris, France, assignors to Franco ChemieS.a.r.l., Paris, France No Drawing. Continuation of abandonedapplication Ser. No. 798,180, Feb. 10, 1969. This application Jan. 18,1972, Ser. No. 218,850

Claims priority, application France, Feb. 16, 1968, 140 204 The portionof the termof the patent subsequent to Oct. 9, 1990, has been disclaimedInt. Cl. A61k 27/00 US. Cl. 424-317 2 Claims ABSTRACT OF THE DISCLOSURELithium parachlorophenoxyacetate is a novel medicament active in thetreatment of mental diseases. It is prepared by reactingparachlorophenoxyacetic acid with lithium carbonate.

This is a continuation of application Ser. No. 798,180 filed Feb. 10,1969, now abandoned.

BACKGROUND AND SUMMARY OF THE INVENTION ing the product thus obtainedwhich is eventually crystallized.

DETAILED DESCRIPTION OF THE INVENTION Lithium parachlorophenoxyacetate(or PC 67.8) is described in greater detail hereinafter:

1. Physico-chemical characteristics-(a) Formula:

c1 -o 011:0 oo Li olHtololm M.W.=192. M.P.=2l0 to 214 C. (capillarytube).

(b) Method of preparing the compound In a one-liter Erlenmeyer flaskequipped with a magnetic stirrer and containing a 62.2 g. suspension ofparachlorophenoxyacetic acid in 200 ml. of water, 12.4 g. of Li CO areadded by small amounts while stirring during about one hour. Aftercompleting the addition of Li CO the mix is stirred until a Clearsolution is obtained; then this solution is evaporated in vacuo and theresulting product is crystallized by using 200 ml. of methanol. Thiscrystallization is facilitated by using a few cc. of ethyl ether. Aftercentrifuging and drying these crystals in vacuo, 50 g. of lithiumparachlorophenoxy-acetate are obtained.

2. Pharmacological properties-The toxicity of PC 67.8 is relatively low(a 50 l. d. calculated during 5 days with mice amounted to 1,600mg./kg.).

The conventional tests for studying the psychomotive behavior in theanimal were used, notably the examination of the behavior of an animalplaced in a new environment (cylindrical box or perforated board).

The time required for exploring the new environment, the number ofpassages of the animal across the beam of photoelectric cells, thenumber of holes explored by the animal with its muzzle, constituted theessential parameters whereby the activity of PC 67.8 was converted intostatistical figures. Throughout these tests a sedative an antiolyticaction was observed.

These studies were completed by the X-ray encephalographic examinationwhich confirmed the results and proved in addition that the reactions topropioceptive stimulations were extended.

3. Therapeutic applications-The above-described products were utilizedin the treatment of psychiatric diseases of the depressive type, andalso of certain psychoses, notably the maniaco-depressive psychosis.

4. Pharmaceutic forms.The products may be administered by the oralroute, or in the form of injections, by the rectal route, or in anypharmaceutically acceptable form.

The useful dose of the active products for human therapy should be aneffective non-toxic amount within the range of from to 500 mg. per day,according to cases.

What we claim is:

1. A method of treating psychiatric diseases of the depressive type andmaniaco-depressive psychosis consisting of administering to a human apharmaceutically acceptible form supplying daily from 100 to 500milligrams of lithium parachlorophenoxyacetate, said administrationbeing orally, by injection or rectally.

2. A method of controlling psychomotive behavior consisting ofadministering to an animal an eifective amount for said control oflithium parachlorophenoxyacetate.

References Cited Chem. Abst., 63, 13117b (1965). Chem. Abst., 59, 2082a(1963 Gersham, Amer. J. Psychiat., 124210, April 1968, pp. 1452-56.

STANLEY J. FRIEDMAN, Primary Examiner 9 -U1 I1TEI STATES PATENT OFFICECERTIFICATE OF CORRECTIQNI Patent No. 3,803, 322 Dated April 9, 1974fls) 5i Jeen-Claude Denis andJerome Rambaud It is certified that errorappears in the above-identified patent and that said Letters Patent arehereby corrected as shown below:

On the title page, column 1, line 23, after "filed Feb. 10, 1969,del'ete "now abandoned and insert -now U'.S. Patent No.-

Signed and eeale d this 18th day of February 1975.

(SEAL) Attest: f

' C. MARSHALL DANN RUTH C. MASON Attesting Officer.

Commissioner of Patents 9. and Trademarks

